Cayman Fluticasone Propionate

Fluticasone propionate is a synthetic corticosteroid and glucocorticoid receptor agonist. It inhibits AP-1-mediated transcription in a transrepression assay using ChaGo-K-1 cells (IC₅₀ = 0.04 nM). Fluticasone propionate selectively binds to the glucocorticoid receptor (IC₅₀ = 0.0009 µM) over the progesterone, mineralocorticoid, and androgen receptors (IC₅₀s = 0.021, 0.149, and >10 µM, respectively), as well as estrogen receptor α (ERα) and ERβ (IC₅₀s = >10 µM for both). It increases apoptosis of T cells isolated from human peripheral blood in a concentration-dependent manner and induces spontaneous apoptosis of primary human eosinophils (EC₅₀ = 3.7 nM).^, Fluticasone propionate completely inhibits congestion in a guinea pig model of allergic rhinitis induced by ovalbumin when administered as a 0.5 mg/mL solution at 20 µl/nostril. It reduces ovalbumin-induced increases in IL-4 in nasal lavage fluid in the same model. Fluticasone propionate also potentiates voltage-dependent potassium channel 1 (K_v1) currents in an inside-out patch-clamp assay (EC₅₀ = 37 nM). Formulations containing fluticasone propionate have been used in the treatment of allergic and non-allergic rhinitis.

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